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JHU37152 (DREADD ligand)

Product overview

Novel DREADD ligand with high affinity and potency for hM3Dq and hM4Di. Active in vivo. Freebase.

Biological description

JHU37152 is a novel DREADD ligand with high affinity and potency for hM3Dq and hM4Di (Ki values are 1.8 nM (hM3Dq) and 8.7 nM (hM4Di).

It displays high potency and efficacy in fluorescent and BRET-based assays (EC50 values are 5 nM (hM3Dq) and 0.5 nM (hM4Di).

JHU37152 is reported to be a potent in vivo DREADD agonist, selectively inhibiting locomotor activity in D1-hM3Dq and D1-hM4Di mice at doses of 0.01 - 1 mg/kg (i.p), with no significant activity in non-DREADD expressing (wildtype) mice.

JHU37152 also displays high in vivo DREADD occupancy (as measured by displacement of [11]Clozapine DREADD binding in vivo in various species).